Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMRQ4L6)

Drug Name

HHCYH33 Drug Info

Synonyms

CYH33; UNII-RCA38L4HB5; RCA38L4HB5; 1494684-28-4; Methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate; CYH 33; CYH-33; SCHEMBL16622890; BDBM330295; HY-123938; CS-0087546; US9724352, I-33; Carbamic acid, N-(5-(6-((4-(methylsulfonyl)-1-piperazinyl)methyl)-4-(4-morpholinyl)pyrrolo(2,1-F)(1,2,4)triazin-2-yl)-4-(trifluoromethyl)-2-pyridinyl)-, methyl ester; Methyl N-(5-(6-((4-(methylsulfonyl)-1-piperazinyl)methyl)-4-(4-morpholinyl)pyrrolo(2,1-F)(1,2,4)triazin-2-yl)-4-(trifluoromethyl)-2-pyridinyl)carbamate; methyl N-[5-[6-[(4-methylsulfonylpiperazin-1-yl)methyl]-4-morpholin-4-ylpyrrolo[2,1-f][1,2,4]triazin-2-yl]-4-(trifluoromethyl)pyridin-2-yl]carbamate

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 1	[1]

Cross-matching ID

PubChem CID: 72550012
CAS Number: CAS 1494684-28-4
TTD Drug ID: DMRQ4L6

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting PI3-kinase alpha (PIK3CA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[3]
Alpelisib	DMEXMYK	Breast cancer	2C60-2C65	Approved	[4]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[5]
GDC-0032	DMT4QHD	Breast cancer	2C60-2C65	Phase 3	[6]
LY3023414	DMD9KYF	Prostate cancer	2C82.0	Phase 2	[7]
PA-799	DMLSYJQ	Colorectal cancer	2B91.Z	Phase 1/2	[8]
MLN1117	DMCVBQD	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
PWT-33597	DMJY15D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
BLY719	DMYHNV3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
LY3849524	DM8I68X	Breast cancer	2C60-2C65	Phase 1	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase alpha (PIK3CA)	TTEUNMR	PK3CA_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT04856371) Study of CYH33 in Combination With Endocrine Therapy With or Without Palbociclib in Patients With HR+, HER2- Advanced Breast Cancer. U.S. National Institutes of Health.
2	Adaptive resistance to PI3Kalpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. Cell Death Dis. 2021 Jan 14;12(1):85.
3	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
5	Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
6	Company report (BioOncology)
7	Company report (Lilly)
8	The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
9	National Cancer Institute Drug Dictionary (drug id 714372).
10	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
11	In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer. Anticancer Res. 2015 Jan;35(1):175-82.
12	ClinicalTrials.gov (NCT05307705) A Study of LOXO-783 Administered as Monotherapy and in Combination With Anticancer Therapies for Patients With Advanced Breast Cancer and Other Solid Tumors With a PIK3CA H1047R Mutation. U.S.National Institutes of Health.